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Targeting Cerebral Muscarinic Acetylcholine Receptors with Radioligands for Diagnostic Nuclear Medicine Studies

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Ion Channel Localization

Part of the book series: Methods in Pharmacology and Toxicology ((MIPT))

Abstract

Nerve cells communicate via the release of chemical messengers (neurotransmitters) which bind to a site (receptor) on another or the same cell causing an effect. The various neuroreceptor classes are responsible for important functions such as movement, memory, and learning. Naturally occurring neurotransmitters are agonists, molecules that trigger an effect in the target cell after binding to the receptor site. In most cases, the binding period of an agonist to the receptor is short and after release from the receptor, the agonist is rapidly taken up by the same nerve cell (reuptake) or metabolized by various bioenzymes. Antagonists are artificial “false” neurotransmitters that bind to a receptor, often with similar or higher affinity compared to an agonist, but do not cause an effect in the target receptor other than preventing the binding of the agonist. Typically, antagonists are designed to increase the binding affinity to the receptor site, to delay release from the receptor pocket, and inhibit the metabolism by bioenzymes.

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Authors and Affiliations

  1. Nuclear Medicine Group, Life Sciences Division, Oak Ridge National Laboratory, Oak Ridge, TN

    Daniel W. McPherson

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  1. Daniel W. McPherson
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Editors and Affiliations

  1. University of Michigan, Ann Arbor, MI

    Anatoli N. Lopatin

  2. Washington University Medical School, St. Louis, MO

    Colin G. Nichols

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© 2001 Humana Press Inc. Totowa, NJ

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W. McPherson, D. (2001). Targeting Cerebral Muscarinic Acetylcholine Receptors with Radioligands for Diagnostic Nuclear Medicine Studies. In: Lopatin, A.N., Nichols, C.G. (eds) Ion Channel Localization. Methods in Pharmacology and Toxicology. Humana Press. https://doi.org/10.1385/1-59259-118-3:17

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  • DOI: https://doi.org/10.1385/1-59259-118-3:17

  • Publisher Name: Humana Press

  • Print ISBN: 978-0-89603-833-2

  • Online ISBN: 978-1-59259-118-3

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